On the Chemistry of Phorbol, XIX [1] Preparation of Tritium-Labelled 12-O-RetinoyIphorbol-13-acetate([20-3H]-RPA)
2014
Tremp, G. L. | Hecker, E.
In contrast to established principles of radioactive labelling of diterpene esters such as TPA it was impossible to introduce tritium into the highly sensitive 12-0-retinoylphorbol-13-acetate (RPA) via reduction of its cold 20-aldehyde with [³H]-sodium borohydride. As an alternative successful procedure, [20-³H]-phorbol-13-acetate was prepared at first. It was protected in position 20 by reaction with tritylchloride and the tritylether reacted with retinoic acid. In both reactions appropriate phorbol acetates were used as easy to separate cold carriers. After removal of the 20-tritylether group, [20-³H]-RPA of a specific activity was obtained that was sufficient for the compound to be used as a tool in biochemical investigations
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